Silley P, Griffiths J W, Monsey D, Harris A M
Chemotherapy Department, Glaxo Group Research Limited, Greenford, United Kingdom.
Antimicrob Agents Chemother. 1990 Sep;34(9):1806-8. doi: 10.1128/AAC.34.9.1806.
GR69153 is a novel cephalosporin incorporating a catechol-substituted 7-aminothiazolyl-oxime. The antibiotic is actively transported into gram-negative cells via iron-regulated outer membrane proteins regulated by the tonB product. This transport enhances bactericidal activity most significantly at low concentrations, essentially removing the permeability barrier for antibiotic uptake.
GR69153是一种新型头孢菌素,其包含一个儿茶酚取代的7-氨基噻唑肟。该抗生素通过由tonB产物调控的铁调节外膜蛋白被主动转运至革兰氏阴性菌细胞内。这种转运在低浓度时最显著地增强杀菌活性,基本消除了抗生素摄取的通透性屏障。